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Q8 Assignment By Lauren McCormick (Lipitor (atorvostatin)…
Q8 Assignment
By Lauren McCormick
Lipitor (atorvostatin)
Pharmacokinetics
Dosage
Initial: 10-20mg 1x/day, orally
Range: 10-80mg 1x/day
Adjustment interval: 2-4 weeks
Half-life
Parent Drug: ~14 hours
Metabolites: 20-30 hours
Duration of action
Time to peak, serum: 1-2 hours
Initial onset: 3-5 days
Maximum reduction: 2-4 weeks
Metabolism
Hepatic via CYP3A4
Excretion
In bile, following hepatic metabolism
In urine, unchanged drug (<2%)
Indication
Prevention of cardiovascular disease -
patient's indication
Reduce risk of MI, stroke in patients with high risk (age, HTN, high cholesterol)
Contraindication
Hypersensitivity to atorvostatin
Active liver disease
Unexplained persistent elevations of serum transaminases
Pregnancy, breastfeeding
Cost
Average retail: $12.58 per 10mg tablet
Mechanism of Action
reduces production of mevalonic acid from HMG-CoA
compensatory increase in expression of LDL receptors on hepatocyte membranes & stimulation of LDL catabolism
Inhibits HMG-CoA reductase
(rate limiting enzyme in cholesterol synthesis)
also....
improves endothelial function
reduces inflammation at site of coronary plaque
inhibits platelet aggregation
anti-coagulation effects
Potential Mild Interaction
Avodart (dutasteride)
Mechanism of Action
4-azo analog of testosterone
competitive & selective inhibitor of reproductive tissues & skin and hepatic 5alpha-reductase
inhibits conversion of testosterone to dihydrotestosterone
suppresses serum dihydrotestosterone levels
Pharmacokinetics
Dosage
Males: 0.5mg 1x/day, orally
(alone or in combo w/ tamsulosin)
Half-life
Terminal: ~5 weeks
(Half-life increases with age)
Duration of action
Time to peak: 2-3 hours
Metabolism
Hepatic via CYP3A4, CYP3A5
Excretion
In feces: 40% metabolites, 5% unchanged drug
In urine: <1% unchanged drug
~55% of dose unaccounted for
Indication
Benign prostatic hyperplasia (BPH)
(Enlarged Prostate) -
patient's indication
to improve symptoms, reduce risk of acute urinary retention, reduce risk of surgery
Contraindication
hypersensitivity to dutasteride & other 5-alpha-reductase inhibititors
use in pediatric patients
women of childbearing potential, pregnancy
Cost
Average retail: $6.05 per 0.5mg tablet
Dabigatran Etexilate
(Pradaxa)
Mechanism of Action
Prodrug lacks anticoagulant activity
converted to active dabigatran
this is a reversible, direct thrombin inhibitor
inhibits free and fibrin-bound thrombin
inhibits coagulation by preventing thrombin-mediated effects
blocks cleavage of fibrinogen to fibrin, activation of factors V, VIII, XI, XIII, and inhibition of platelet aggregation
Pharmacokinetics
Duration of action
rapid absorption
1hr to peak plasma concentrations
Metabolism
Dabigatran etexilate (prodrug)
: hydrolyzed to dabigatran by plasma & hepatic esterases
Dabigatran (active drug)
: Hepatic glucuronidation
Half-life
Typically 12-17 hours
Excretion
80% in urine
Dosage
150mg 2x/day, orally
Indication
Deep venous thrombosis, pulmonary embolism treatment & prevention
Nonvalvular atrial fibrillation-
patient's indication
VTE prophylaxis in total hip arthroplasty
Contraindication
Hypersensitivity to dabigatran
active pathological bleeding
patients with mechanical prosthetic heart valves
Cost
Average Retail: $8.65 per 75mg tablet
Metoprolol
Mechanism of Action
selective inhibitor (competitive blocking) of beta1 adrenergic receptors
little to no effect on beta2 adrenergic receptors
Indication
angina
Hypertension -
patient's indication
myocardial infarction
heart failure w/ reduce ejection fraction
Contraindication
cardiogenic shock
sinus bradycardia
overt heart failure
sick sinus syndrome
Pharmacokinetics
Dosage
Immediate release
(metoprolol tartrate)
for HTN
Initial: 50mg 2x/day, orally
titrate weekly
Max daily dosage: 400mg/day
Extended release
(metoprolol succinate)
for HTN
Initial: 25-100mg 1x/day, orally
titrate weekly
Max daily dosage: 400mg/day
Half-life
Adults: 3-4 hours
7-9 hours for hepatic impaired patients
Duration of action
Oral, Immediate release:
50% reduction in max heart rate after single dose:
50mg --> 5 hours
20mg --> 3.3 hours
100mg --> 6.4 hours
Extended release:
~24 hours
Metabolism
Exclusively hepatic via CYP2D6
50% via first-pass effect
Excretion
95% in urine
5-10% unchanged drug (30-40% in hepatic impaired patients)
Cost
Average Retail Price: $1.05 - $1.28 per 25mg tablet
Finasteride
Mechanism of Action
inhibits type II 5-alpha reductase
inhibition of conversion of testosterone to dihydrotestosterone
suppresses serum dihydrotestosterone levels
Indication
benign prostatic hyperplasia -
patient's indication
androgenetic alopecia
Contraindication
hypersensitivity to finasteride
pregnancy or women of childbearing potential
Cost
Average Retail Price: $0.47 - $3.19 per 5mg tablet
Pharmacokinetics
Dosage
For benign prostatic hyperplasia:
5mg 1x/day, orally for 6 months
Half-life
5-6 hours in adults
8 hours in elderly
Duration of action
Dihydrotestosterone levels return to normal within 14 days of discontinuation of treatment
Metabolism
Hepatic via CYP3A4
Excretion
57% feces
39% urine as metabolites
Metformin (diabetes)
Pharmacokinetics
Dosage
Immediate Release
Initial: 500mg 1-2x/day or 850mg 1x/day
Maintenance Dose: 1g 2x/day or 850mg 2x/day
Extended Release
Initial: 500mg-1g 1x/day
Half-life
Plasma: 4-9hrs
Blood: ~17.6hrs
Duration of action
Onset of action within days;
Max effects up to 2 weeks
Metabolism
Not metabolized by the liver.
Excretion
90% unchanged in urine
Indication
Diabetes mellitus, type 2 -
patient's indication
Contraindication
hypersensitivity to metformin
severe renal dysfunction
acute or chronic metabolic acidosis
Cost
Average Retail Price: $0.75 - $1.03 per 500mg tablet
Mechanism of Action
decreases hepatic glucose production
decreases intestinal absorption or glucose & improves insulin sensitivity
increases peripheral glucose uptake & utilization
severe peripheral arterial circulatory disorders
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